Abstract
The types of interaction of exogenous ligands of the GABAA transmitter system, which influence different subunits of the GABA-benzodiazepine—receptor complex (RC), were studied under conditions when the level of an endogenous transmitter was changed. The effector analysis showed that some types of ligands of the GABA-RC interact in a cooperative manner. Hyperbolic (benzodiazepines) and linear (barbiturates) dose—effect dependences were observed, and cooperativity coefficients between the effects of the ligand complexes and the number of their binding sites on one of the four elements of a GABA-RC structural model correspond to each other. It was shown that the effects of muscimol changed their direction under conditions of a deficiency of endogenous transmitter, which allows us to characterize muscimol as a partial agonist. The GABA-mimetic properties of ethanol are manifested not only in weakening of thiosemicarbazide-induced convulsive effects, but also in an increase in its lethal dose.
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